EPZ011989 free base · Synonyms: EPZ-011989 · EPZ 011989
EPZ011989 is a potent and orally active Zeste Homolog 2 inhibitor.
For research use only. Not for human or veterinary use.
EPZ011989 structure
CAS No.: 1598383-40-4
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 250 mg | USD 785.00 | BP-02335-250mg | In stock | Get quote |
| 500 mg | USD 1,250.00 | BP-02335-500mg | In stock | Get quote |
| 1 g | USD 1,800.00 | BP-02335-1g | In stock | Get quote |
| 2 g | USD 3,200.00 | BP-02335-2g | In stock | Get quote |
| 5 g | Inquire | BP-02335-5g | In stock | Inquire |
Need another size or custom synthesis? Request a quote.
Description
EPZ011989 is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ011989 has inhibitory inhibition for EZH2 with a Ki value of <3 nM.
Biological activity
EPZ011989 is also a specific EZH2 inhibitor with a >15-fold selectivity over EZH1 and >3000-fold selectivity relative to the Ki of 20 other histone methyltransferases (HMTs) tested. EPZ011989 reduces cellular H3K27 methylation in the Y641F, mutant-bearing human lymphoma cell line, WSU-DLCL2, with an IC50 below 100 nM. EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma.
Identifiers
- SMILES
-
CCN([C@H]1CC[C@@H](CC1)N(C)CCOC)C1=C(C)C(=CC(=C1)C#CCN1CCOCC1)C(=O)NCC1=C(C)C=C(C)NC1=O - InChIKey
-
XQFINGFCBFHOPE-WXUXXXNLSA-N
Specifications
- MW (average)
- 605.8105
- Formula
- C35H51N5O4
- CAS No.
- 1598383-40-4
- Physical state
- Solid
- Color
- Light yellow to yellow
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder -20℃ 2 years; In solvent -20℃ 1 month;
Solubility
Soluble in DMSO